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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
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Encapsulation of exemestane in polycaprolactone nanoparticles: optimization, characterization, and release kinetics
Abhinesh Kumar1, Krutika Sawant1
1Drug Delivery Research Laboratory, TIFAC Center of Relevance and Excellence in NDDS, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Shri G.H. Patel Pharmacy Building, Fatehgunj, Vadodara-390002 Gujarat India.
Cancer Nanotechnology
|June 13, 2015
Summary
This study developed exemestane-loaded carboxylated polycaprolactone nanoparticles for sustained intravenous delivery. Optimized nanoparticles achieved high drug entrapment and desired particle size for targeted drug delivery.
Area of Science:
- Polymer Chemistry
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Exemestane (exe) is a steroidal aromatase inhibitor used in cancer therapy.
- Developing effective drug delivery systems is crucial for targeted and sustained therapeutic action.
- Polymeric nanoparticles offer potential for controlled drug release and improved bioavailability.
Purpose of the Study:
- To develop and optimize a polymeric drug delivery system for exemestane (exe) using carboxylated polycaprolactone (cPCL) nanoparticles (NPs).
- To achieve sustained and targeted intravenous delivery of exemestane.
- To statistically optimize the formulation for high percentage drug entrapment (PDE) and controlled particle size (PS).
Main Methods:
- Synthesized carboxylated polycaprolactone (cPCL) via ring-opening polymerization.
- Prepared exe-loaded cPCL NPs using interfacial deposition.
- Employed a Box-Behnken design for optimization of formulation variables (exe/cPCL ratio, cPCL amount, organic phase volume).
- Characterized NPs using FTIR, GPC, DSC, TEM, and in vitro release studies.
Main Results:
- Optimized formulation achieved 83.96% PDE and 180.5 nm PS with desirability of 1.0.
- Fourier transform infrared (FTIR) and gel permeation chromatography (GPC) confirmed successful polymerization.
- Differential scanning calorimetry (DSC) indicated no drug-polymer interaction.
- Transmission electron microscopy (TEM) showed spherical, non-aggregated NPs.
- In vitro release studies demonstrated sustained drug release following the Korsmeyer-Peppas model (Fickian diffusion).
- Zeta potential was -33.8 ± 2.1 mV, indicating formulation stability.
Conclusions:
- Statistically optimized exemestane-loaded cPCL NPs with high drug entrapment and suitable particle size were successfully developed.
- The developed NPs are promising for sustained intravenous delivery and passive targeting.
- Box-Behnken design is an effective tool for optimizing nanoparticle formulations for drug delivery.
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